小分子药物在中重度溃疡性结肠炎中的治疗进展

doi:10.12092/j.issn.1009-2501.2026.03.011

摘要/Abstract

摘要：

溃疡性结肠炎（ulcerative colitis，UC）是一种主要影响结肠和直肠的慢性非感染性炎症，其特点是肠道黏膜层的连续性炎症和溃疡形成。近年来，随着对UC发病机制的深入研究，UC的治疗策略逐渐转向分子水平的精准靶向治疗。小分子药物因其独特的优势，如给药方便、无免疫原性、半衰期短等，在中重度UC的治疗中展现出重要潜力。本文综述了小分子药物在中重度UC中的治疗进展，重点介绍了近年来有代表性的小分子药物及其临床试验结果。

关键词: 中重度溃疡性结肠炎, 小分子药物, JAK/STAT信号通路, S1P/S1PR信号通路

Abstract:

Ulcerative colitis (UC) is a chronic non-infectious inflammation primarily affecting the colon and rectum, characterised by continuous inflammation and ulceration of the intestinal mucosal layer. In recent years, with deepening research into the pathogenesis of UC, treatment strategies have progressively shifted towards precision targeted therapy at the molecular level. Small-molecule drugs, owing to their distinct advantages such as convenient administration, lack of immunogenicity, and short half-life, demonstrate significant potential in the treatment of moderate-to-severe UC. This review summarises therapeutic advances in small-molecule drugs for moderate-to-severe UC, focusing on representative compounds and their clinical trial outcomes in recent years.

Key words: moderate-to-severe ulcerative colitis, small-molecule drugs, JAK/STAT signalling pathway, S1P/S1PR signalling pathway

中图分类号:

R574.1
R969

王福蕊, 黄田, 蒋雯莉, 胡泽楠. 小分子药物在中重度溃疡性结肠炎中的治疗进展[J]. 中国临床药理学与治疗学, 2026, 31(3): 392-399.

Furui WANG, Tian HUANG, Wenli JIANG, Zenan HU. Therapeutic advances in small-molecule drugs for moderate-to-severe ulcerative colitis[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2026, 31(3): 392-399.

图/表 3

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药物名称	作用机制	用法	获批情况	全球阶段	中国阶段
Tofacitinib	JAK抑制剂	口服	中重度UC（2018，FDA）	批准上市	暂未发现相关报道
Filgotinib	选择性JAK1抑制剂	口服	中重度UC（2021，EMA）	批准上市	Ⅲ期临床
Upadacitinib	选择性JAK1抑制剂	口服	中重度UC（2022，FDA）	批准上市	批准上市
Ozanimod	S1PR调节剂	口服	中重度UC（2021，FDA）	批准上市	批准上市
Etrasimod	S1PR调节剂	口服	中重度UC（2023，FDA）	批准上市	Ⅲ期临床

药物名称	作用机制	用法	获批情况	全球阶段	中国阶段
Tofacitinib	JAK抑制剂	口服	中重度UC（2018，FDA）	批准上市	暂未发现相关报道
Filgotinib	选择性JAK1抑制剂	口服	中重度UC（2021，EMA）	批准上市	Ⅲ期临床
Upadacitinib	选择性JAK1抑制剂	口服	中重度UC（2022，FDA）	批准上市	批准上市
Ozanimod	S1PR调节剂	口服	中重度UC（2021，FDA）	批准上市	批准上市
Etrasimod	S1PR调节剂	口服	中重度UC（2023，FDA）	批准上市	Ⅲ期临床